In vitro identification of the human cytochrome P450 enzymes involved in the metabolism of R(+)- and S(-)-carvedilol.

@article{Oldham1997InVI,
  title={In vitro identification of the human cytochrome P450 enzymes involved in the metabolism of R(+)- and S(-)-carvedilol.},
  author={Harriet G. Oldham and Stephen E. Clarke},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={1997},
  volume={25 8},
  pages={970-7}
}
Both the R(+) and the S(-) enantiomers of carvedilol were metabolized in human liver microsomes primarily to 4'- (4OHC) and 5'-(5OHC) hydroxyphenyl, 8-hydroxy carbazolyl (8OHC) and O-desmethyl (ODMC) derivatives. The S(-) enantiomer was metabolized faster than the R(+) enantiomer although the same P450 enzymes seemed to be involved in each case. A combination of multivariate correlation analysis, the use of selective inhibitors of P450, and microsomes from human lymphoblastoid cells expressing… CONTINUE READING